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      News & Perspective Drugs & Diseases CME & Education Academy Video Decision Point
      Drugs & Diseases > General Surgery

      Hepatocellular Carcinoma (HCC) Medication

      Updated: Dec 07, 2022
      • Author: Luca Cicalese, MD, FACS; Chief Editor: John Geibel, MD, MSc, DSc, AGAF  more...
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      Medication

      Medication Summary

      Few systemic options exist for patients with unresectable hepatocellular carcinoma (uHCC). The combination of tremelimumab plus durvalumab is the first dual checkpoint combination approved showing improved efficacy compared with monotherapy. Sorafenib monotherapy or durvalumab monotherapy are indicated for patients with unresectable or advanced HCC. Other recent options are regorafenib, nivolumab, lenvatinib, pembrolizumab, cabozantinib, and ramucirumab.

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      Antineoplastics, Tyrosine Kinase Inhibitor

      Class Summary

      Tyrosine kinase inhibitors have shown inhibitory activity of membrane-bound and intracellular kinases involved in normal cellular functions and in pathological processes.

      Sorafenib (Nexavar)

      Sorafenib is a tyrosine kinase inhibitor. It is indicated for unresectable hepatocellular carcinoma.

      Regorafenib (Stivarga)

      Regorafenib is a tyrosine kinase inhibitor. It is indicated for hepatocellular carcinoma in patients who have been previously treated with sorafenib.

      Cabozantinib (Cabometyx)

      Cabozantinib is an inhibitor of multiple tyrosine kinases, including RET, MET, and VEGFR-2. It is indicated for HCC in patients previously treated with sorafenib.

      Selpercatinib (Retevmo)

      Selpercatinib is a kinase inhibitor of wild-type rearranged during transfection (RET) and multiple mutated RET isoforms, as well as vascular endothelial growth factor receptors (VEGFR1, VEGFR3). The FDA granted accelerated approval to selpercatinib (Retevmo) for adults with locally advanced or metastatic solid tumors with a rearranged during transfection (RET) gene fusion that have progressed on or following prior systemic treatment or who have no satisfactory alternative treatment options.

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      Antineoplastics, VEGF Inhibitor

      Class Summary

      Inhibits the kinase activities of various subtypes of vascular endothelial growth factor (VEGF) receptors.

      Lenvatinib (Lenvima)

      Lenvatinib is a receptor tyrosine kinase (RTK) inhibitor that inhibits the kinase activities of VEGFR1 (FLT1), VEGFR2 (KDR), and VEGFR3 (FLT4). It also inhibits other RTKs that have been implicated in pathogenic angiogenesis, tumor growth, and cancer progression in addition to their normal cellular functions, including fibroblast growth factor (FGF) receptors FGFR1, 2, 3, and 4; the platelet-derived growth factor receptor alpha (PDGFR-α); KIT; and RET. It is indicated for first-line treatment of unresectable HCC.

      Ramucirumab (Cyramza)

      Vascular endothelial growth factor receptor 2 (VEGFR2) antagonist that specifically binds VEGF receptor 2 and blocks binding of VEGFR ligands, VEGF-A, VEGF-C, and VEGF-D. As a result, ramucirumab inhibits ligand-stimulated activation of VEGF2, thereby inhibiting ligand-induced proliferation, and migration of human endothelial cells. It is indicated as monotherapy for hepatocellular carcinoma (HCC) in patients with alpha fetoprotein (AFP) of 400 ng/mL or higher who have been previously treated with sorafenib.

      Bevacizumab (Avastin, Bevacizumab-awwb, Mvasi)

      Recombinant humanized monoclonal antibody to VEGF. It blocks the angiogenic molecule VEGF thereby inhibiting tumor angiogenesis, starving tumor of blood and nutrients. It is indicated, in combination with atezolizumab, for unresectable or metastatic HCC who have not received prior systemic therapy.

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      PD-1/PD-L1 Inhibitors

      Class Summary

      PD-1 and related target PD-ligand 1 (PD-L1) are expressed on the surface of activated T cells under normal conditions. PD-L1/PD-1 interaction inhibits immune activation and reduces T-cell cytotoxic activity when bound.

      Nivolumab (Opdivo)

      Nivolumab is a programmed death receptor-1 (PD-1) blocking antibody. FDA granted accelerated approval to combination of nivolumab and ipilimumab for HCC in patients previously treated with sorafenib. It was previously also indicated as a single-agent for patients who have been previously treated with sorafenib. However, indication was voluntarily withdrawn in the U.S. by manufacturer based on failure of showing a statistically significant benefit in overall survival compared to nivolumab and sorafenib combined.

      Pembrolizumab (Keytruda)

      Pembrolizumab is a monoclonal antibody that binds to the PD-1 receptor and blocks its interaction with PD-L1 and PD-L2, releasing PD-1 pathway-mediated inhibition of the immune response, including the antitumor immune response. Binding of PD-1 ligands, PD-L1 and PD-L2, to the PD-1 receptor found on T cells, inhibits T cell proliferation and cytokine production. It is indicated for patients with hepatocellular carcinoma (HCC) who have been previously treated with sorafenib.

      Atezolizumab (Tecentriq)

      Monoclonal antibody to programmed cell death ligand-1 protein (PDL1). It binds to PDL-1 which blocks the interaction between PDL-1 and its ligands. It is indicated, in combination with bevacizumab, for unresectable or metastatic HCC who have not received prior systemic therapy.

      Dostarlimab (Dostarlimab-gxly, Jemperli)

      Dostarlimab is a humanized monoclonal antibody of the IgG4 isotype binds to PD-1 receptor and blocks its interaction with PD-L1 and PD-L2, releasing PD-1 pathway–mediated inhibition of the immune response, including antitumor immune response

      The binding of PD-1 ligands, PD-L1 and PD-L2 to PD-1 receptor found on T-cells. It inhibits T-cell proliferation and cytokine production. It is indicated for adults with mismatch repair-deficient (dMMR) recurrent or advanced endometrial cancer that has progressed on or following a prior platinum-containing regimen.

      Durvalumab (Imfinzi)

      Durvalumab is a human IgG1 kappa monoclonal antibody that blocks PD-L1 binding to PD-1 and CD80, and therefore overcoming/preventing PD-L1-mediated inhibition/suppression of T-cell activation. It is Indicated in combination with tremelimumab for unresectable hepatocellular carcinoma (uHCC).

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      Antineoplastics, Anti-CTLA4 Antibodies

      Class Summary

      Cytotoxic T-lymphocyte-associated antigen 4 (CTLA-4) blocking monoclonal antibody blocks the interaction with its ligands CD80 and CD86. This action releases CTLA-4-mediated inhibition of T-cell activation.

      Tremelimumab (Imjudo, Tremelimumab-actl)

      Tremelimumab is a cytotoxic T-lymphocyte-associated antigen 4 (CTLA-4) blocking human IgG2monoclonal antibody, produced by recombinant DNA technology in NS0 cell suspension culture and has a molecular weight of 149 kD. The monoclonal antibody binds to CTLA-4 and blocks the interaction with its ligands CD80 and CD86, releasing CTLA-4-mediated inhibition of T-cell activation. It is Indicated in combination with tremelimumab for uHCC.

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